Indole-glucosides as novel sodium glucose co-transporter 2 (SGLT2) inhibitors. Part 2

Xiaoyan Zhang; Maud Urbanski; Mona Patel; Geoffrey G Cox; Roxanne E Zeck; Haiyan Bian; Bruce R Conway; Mary Pat Beavers; Philip J Rybczynski; Keith T Demarest

doi:10.1016/j.bmcl.2005.12.006

Indole-glucosides as novel sodium glucose co-transporter 2 (SGLT2) inhibitors. Part 2

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1696-701. doi: 10.1016/j.bmcl.2005.12.006. Epub 2005 Dec 27.

Authors

Xiaoyan Zhang¹, Maud Urbanski, Mona Patel, Geoffrey G Cox, Roxanne E Zeck, Haiyan Bian, Bruce R Conway, Mary Pat Beavers, Philip J Rybczynski, Keith T Demarest

Affiliation

¹ Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 1000 Rt. 202, PO Box 300, Raritan, NJ 08869, USA. xzhang11@prdus.jnj.com

PMID: 16380256
DOI: 10.1016/j.bmcl.2005.12.006

Abstract

A series of indole-O-glucosides and C-glucosides was synthesized and evaluated in SGLT1 and SGLT2 cell-based functional assays. Compounds 2a and 2o were identified as potent SGLT2 inhibitors and screened in ZDF rats.

Publication types

Comparative Study

MeSH terms

Animals
Diabetes Mellitus, Experimental / urine
Glucose / metabolism
Glucosides / chemical synthesis
Glucosides / chemistry*
Glucosides / pharmacology*
Indoles / chemistry*
Molecular Structure
Rats
Rats, Zucker
Sodium-Glucose Transporter 1 / antagonists & inhibitors
Sodium-Glucose Transporter 2 Inhibitors*

Substances

Glucosides
Indoles
Sodium-Glucose Transporter 1
Sodium-Glucose Transporter 2 Inhibitors
indole
Glucose